6219-54-1Relevant academic research and scientific papers
[1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINES
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Page/Page column 323, (2021/02/19)
The present invention covers [1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds of general formula (I) in which R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.
Discovery of novel 2,4-diarylaminopyrimidine derivatives as potent and selective epidermal growth factor receptor (EGFR) inhibitors against L858R/T790M resistance mutation
Yan, Qi,Chen, Yuzhe,Tang, Baiyou,Xiao, Qiang,Qu, Rong,Tong, Linjiang,Liu, Jian,Ding, Jian,Chen, Yi,Ding, Ning,Tan, Wenfu,Xie, Hua,Li, Yingxia
, p. 298 - 306 (2018/05/22)
A series of novel 2,4-diarylaminopyrimidine derivatives of AZD9291 were discovered as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors. The majority of these compounds exhibited moderate to excellent EGFR T790 M/L858R inhibitory activities and comparable anti-proliferative activities against double mutant over-expressed NCI-H1975 cells to that of AZD9291. The most promising compounds 8a displayed an IC50 of 4.1 nM against EGFR L858R/T790M mutants. 8a also showed excellent cytotoxic effect against NCI-H1975 cells with an IC50 of 59 nM and 100-fold selectivity over wide-type EGFR over-expressed A431 cells. Compound 8a significantly inhibited tumor growth in NCI-H1975 xenograft models at a non-toxic dose. Docking study performed for 8a with ATP binding site of EGFR-TK showed the similar binding mode to that of AZD9291. All these results suggested that compound 8a was a potential mutant-selective EGFR inhibitor.
Imidazoline derivatives as alpha-1A adrenoceptor ligands
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Page/Page column 35, (2010/02/11)
Compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof are disclosed. Such compounds are useful in the treatment of Alpha-1A mediated diseases or conditions such as urinary incontinence.
2-(Anilinomethyl)imidazolines as α1 adrenergic receptor agonists: α1a subtype selective 2′-heteroaryl compounds
Speake, Jason D.,Navas III, Frank,Bishop, Michael J.,Garrison, Deanna T.,Bigham, Eric C.,Hodson, Stephen J.,Saussy, David L.,Liacos, Jim A.,Irving, Paul E.,Sherman, Bryan W.
, p. 1183 - 1186 (2007/10/03)
The structure-activity relationship of 2′-pyrrole, pyrazole and triazole substituted 2-(anilinomethyl)imidazolines as α1 adrenergic agonists was investigated. The size and orientation of substituents, as well as the position of the heteroatoms, were found to have a profound effect on the potency and selectivity of the molecules. Potent α1A subtype selective agonists have been identified.
